| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
κ Opioid Receptor/KOR
kappa-opioid receptor (KOR). DIPPA hydrochloride is an irreversible antagonist that binds covalently to the kappa-opioid receptor, producing long-lasting blockade. It is selective for KOR over micro and delta opioid receptors, although the exact selectivity ratios are not specified. |
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| ln Vitro |
Specific in vitro binding affinities (IC50 or Ki values) are not reported in the literature. DIPPA is known to be a high-affinity, selective KOR antagonist that binds irreversibly, resulting in long-lasting receptor blockade. It is used primarily for its in vivo activity as a tool to study the physiological and behavioral roles of KOR without requiring continuous administration.
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| ln Vivo |
In Wistar Kyoto rats, DIPPA (2.5 and 5 mg/kg; sc) hydrochloride reduces the latency to feed; however, therapy had no effect on approach latencies in SD rats[2]. The high dose of DIPPA (1 and 5 mg/kg; sc) hydrochloride causes an increase in immobility in SD rats as compared to the group of rats treated with saline[2]. Compared to the 5 mg/kg group of Wistar Kyoto rats, SD rats consume less DIPPA (5 mg/kg) hydrochloride. In both strains, DIPPA hydrochloride dramatically reduces burying time. Burying is reduced in both strains by DIPPA hydrochloride (5 mg/kg) as compared to the within-strain control groups. In SD rats, DIPPA hydrochloride tends to reduce consumption in the home cage but dramatically boosts feeding in the novel cage, where possible anxiolytic-like effects of the substance may counteract its hypophagic effects[2].
In vivo, DIPPA hydrochloride (2.5 and 5 mg/kg; s.c.) decreases the latency to feed in Wistar Kyoto rats but does not alter approach latencies in Sprague Dawley rats. DIPPA (1 and 5 mg/kg; s.c.) at high dose increases immobility in Sprague Dawley rats compared to saline-treated controls. DIPPA (5 mg/kg) decreases burying time in both rat strains. DIPPA can be used for the research of anxiety and antidepressant effects. These effects are mediated by irreversible blockade of KOR. |
| Enzyme Assay |
DIPPA is an irreversible KOR antagonist, so cell-free binding assays typically use a pre-incubation step to allow covalent bond formation. Membranes from CHO-K1 cells expressing human kappa-opioid receptors (or guinea pig brain membranes) are pre-incubated with DIPPA hydrochloride (0.01-10,000 nM) in binding buffer for 60-180 min at 25degC to allow irreversible binding. Unbound compound is removed by washing. Membranes are then incubated with a kappa-selective radioligand (e.g., [3H]-U69,593) under standard equilibrium conditions (60-90 min at 25degC), and the residual specific binding is measured. The degree of irreversible blockade is expressed as percent inhibition of specific binding compared to control. The irreversibility is confirmed by lack of reversibility after extensive washing.
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| Cell Assay |
Cell-based functional assays for KOR: CHO-K1 cells stably expressing human kappa-opioid receptors are pre-incubated with DIPPA (0.1-10,000 nM) for 1-2 hours at 37degC. Cells are then washed extensively to remove unbound compound. After washing, cells are stimulated with a KOR agonist (U50,488 or dynorphin A, 1-100 nM). Functional readouts include inhibition of forskolin-stimulated cAMP accumulation (HTRF assay) or calcium mobilization (FLIPR). The irreversible blockade of KOR is confirmed by persistently reduced agonist responsiveness, even after removal of DIPPA from the medium. Long-lasting antagonism can be assessed over 24-48 hours post-incubation.
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| Animal Protocol |
Animal/Disease Models: Wistar Kyoto rats and SD rats (250–300 g)[2]
Doses: 2.5 and 5 mg/kg Route of Administration: Sc Experimental Results: diminished the latency to feed in Wistar Kyoto rats, but treatment did not alter approach latencies in SD rats. Animal/Disease Models: Wistar Kyoto rats and SD rats (250–300 g)[2] Doses: 1 and 5 mg/kg Route of Administration: Sc Experimental Results: High dose increased immobility in SD rats compared to the saline-treated strain control group. DIPPA hydrochloride is administered subcutaneously (s.c.) to male Wistar Kyoto and Sprague Dawley rats at doses of 1, 2.5, and 5 mg/kg. For feeding behavior tests, latency to feed in a novel environment is measured. For anxiety-like behavior, burying time in the defensive burying test is recorded. For depression-like behavior, immobility time in the forced swim test (FST) is measured. DIPPA (5 mg/kg) produces effects consistent with KOR blockade (reduced burying, increased immobility, reduced feeding latency). The duration of action is prolonged (up to 7 days) due to irreversible binding. Control groups receive vehicle (saline). DIPPA should be used fresh and protected from light. |
| ADME/Pharmacokinetics |
No specific pharmacokinetic data are reported for DIPPA hydrochloride. The molecular weight is 484.87 (C22H24Cl3N3OS). CAS# 155512-52-0. Purity ≥98%. Storage: -20degC, protected from light and moisture. Solubility: DMSO (>10 mg/mL). DIPPA is poorly soluble in water; formulation for in vivo use may require DMSO or co-solvent mixtures. The irreversible binding to KOR results in a long duration of action, with effects lasting several days after a single subcutaneous injection. Clearance, half-life (t1/2), and volume of distribution are not reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for DIPPA hydrochloride. In published animal studies at doses up to 5 mg/kg (s.c.), no signs of acute toxicity (seizures, respiratory depression, severe motor impairment, or mortality) were observed. However, as an irreversible KOR antagonist, DIPPA may have long-lasting effects on KOR-mediated physiological functions, including stress responses, mood, and pain perception. Standard toxicological assessments (hERG, Ames, repeat-dose toxicity) have not been performed. No clinical trials. Not FDA-approved.
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| References |
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| Additional Infomation |
Other information: DIPPA hydrochloride is a research chemical, not FDA-approved. CAS# 155512-52-0. It is an irreversible, long-lasting, selective, and high-affinity kappa-opioid receptor antagonist. DIPPA is useful for studying the role of KOR in neuropsychiatric disorders (anxiety, depression, stress), pain, and addiction. Its long duration of action makes it a valuable tool for prolonged KOR blockade with single administration. Synonyms: DIPPA HCl. For research use only.
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| Molecular Formula |
C22H24CL3N3OS
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|---|---|
| Molecular Weight |
484.87
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| Exact Mass |
483.07
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| CAS # |
155512-52-0
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| PubChem CID |
45073425
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
595
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN([C@H](CN1CCCC1)C2=CC(=CC=C2)N=C=S)C(=O)CC3=CC(=C(C=C3)Cl)Cl.Cl
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| InChi Key |
BNWYENYHNOESCX-ZMBIFBSDSA-N
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| InChi Code |
InChI=1S/C22H23Cl2N3OS.ClH/c1-26(22(28)12-16-7-8-19(23)20(24)11-16)21(14-27-9-2-3-10-27)17-5-4-6-18(13-17)25-15-29;/h4-8,11,13,21H,2-3,9-10,12,14H2,1H3;1H/t21-;/m1./s1
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| Chemical Name |
2-(3,4-dichlorophenyl)-N-[(1S)-1-(3-isothiocyanatophenyl)-2-pyrrolidin-1-ylethyl]-N-methylacetamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0624 mL | 10.3120 mL | 20.6241 mL | |
| 5 mM | 0.4125 mL | 2.0624 mL | 4.1248 mL | |
| 10 mM | 0.2062 mL | 1.0312 mL | 2.0624 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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